新型菊酰胺衍生物的合成修饰及其生物活性

Synthetic Modification and Biological Activities of Novel Chrysanthemum Amide Derivatives

拟菊酯类杀虫剂是合成杀虫剂发展史上继传统有机氯杀虫剂、有机磷杀虫剂、氨基甲酸酯杀虫剂后开发的一种仿生类杀虫剂农药,因具有杀虫谱广、活性高、用量少、环境毒性低等优点而被广泛应用。使用化学合成修饰法,将二溴菊酸与苄胺或多取代苄胺经过N-酰基化反应合成了16个新型菊酰胺衍生物(DCA-01~DCA-16),其结构经1H NMR,13C NMR和MS(ESI)表征。初步的抗蚊杀虫活性测试结果表明:DCA-06对白纹伊蚊幼虫的致死效果最强,其半致死浓度为1.58μM;DCA-06在浓度为1600μg·bottle-1下作用白纹伊蚊雌性成蚊2 h,致死率达到97%。

Pyrethroid is a kind of biomimetic insecticide developed after traditional organochlorine,organophosphorus and carbamate insecticides through the development of synthetic pesticides.It is widely used for having the merits of wide insecticidal spectrum,effective activity,low dosage,low environmental toxicity and etc.This paper synthesized sixteen novel chrysanthemum amide derivatives(DCA-01~DCA-16)through acylation reaction of the benzylamine/poly-substituted benzylamine and the pyrethroid by the method of chemical synthetic modification.The structures were characterized by 1H NMR,13C NMR and MS(ESI).The initial results of the experiment for anti-mosquito activity showed:among these new type of chrysanthemum amides,DCA-06 exhibited strongest mortality effect on Aedes albopictus larvae,and its concentration of semi-mortality was 1.58μM.The killing mortality rate of DCA-06 on female mosquitoes in 1600μg·bottle-1 for 2 h could reach 97%.